Synthesis, structure-activity relationships at the GABAA receptor in rat brain, and differential electrophysiological profile at the recombinant human GABAA receptor of …

B Asproni, G Talani, F Busonero, A Pau…

Index: Asproni, Battistina; Talani, Giuseppe; Busonero, Fabio; Pau, Amedeo; Sanna, Sebastiano; Cerri, Riccardo; Mascia, Maria Paola; Sanna, Enrico; Biggio, Giovanni Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2638 - 2645

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Citation Number: 14

Abstract

A series of new 1, 2-diphenylimidazole derivatives (1a-x) were synthesized and evaluated for their ability to potentiate γ-aminobutyric acid (GABA)-evoked currents in Xenopus laevis oocytes expressing recombinant human GABAA receptors. Many of these compounds enhanced GABA action with potencies (EC50= 0.19-19 μM) and efficacies (maximal efficacies of up to 640%) similar to or greater than those of anesthetics such as etomidate, ...

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